ArticleJournal of medicinal chemistry2013
Synthesis and evaluation of hetero- and homodimers of ribosome-targeting antibiotics: antimicrobial activity, in vitro inhibition of translation, and drug resistance.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 33 citations in OpenAlex.
- Synthesis and antimicrobial activity of molecular hybrids based on eugenol and chloramphenicol pharmacophores.Folia microbiologica · 2023Article
- Functional and Structural Characterization of Diverse NfsB Chloramphenicol Reductase Enzymes from Human Pathogens.Microbiology spectrum · 2022Article
- Investigating the promiscuity of the chloramphenicol nitroreductase from Haemophilus influenzae towards the reduction of 4-nitrobenzene derivatives.Bioorganic & medicinal chemistry letters · 2019Article
- Enhanced of antibacterial activity of antibiotic-functionalized silver nanocomposites with good biocompatibility.Journal of materials science. Materials in medicine · 2019Article
- Derivatives of Ribosome-Inhibiting Antibiotic Chloramphenicol Inhibit the Biosynthesis of Bacterial Cell Wall.ACS infectious diseases · 2018Article
- Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.Chemical Society reviews · 2018Review
- Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors.Molecules (Basel, Switzerland) · 2018Review
- Antimicrobial Activity, AME Resistance, and A-Site Binding Studies of Anthraquinone-Neomycin Conjugates.ACS infectious diseases · 2017Article
- Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions.Antibiotics (Basel, Switzerland) · 2016Review
- Synthesis and antibacterial activity of novel lincomycin derivatives. I. Enhancement of antibacterial activities by introduction of substituted azetidines.The Journal of antibiotics · 2016Article
- Mechanisms of Resistance to Aminoglycoside Antibiotics: Overview and Perspectives.MedChemComm · 2016Article
- Arginine-linked neomycin B dimers: synthesis, rRNA binding, and resistance enzyme activity.MedChemComm · 2016Article
- Synthesis and Biological Activity of Mono- and Di-N-acylated Aminoglycosides.ACS medicinal chemistry letters · 2015Article
- Tobramycin Variants with Enhanced Ribosome-Targeting Activity.Chembiochem : a European journal of chemical biology · 2015Article
- Synthesis and evaluation of chloramphenicol homodimers: molecular target, antimicrobial activity, and toxicity against human cells.PloS one · 2015Article
- New trends in aminoglycosides use.MedChemComm · 2014Article
- Bacterial Enzymes and Antibiotic Resistance.Acta naturaeArticle
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
In this study, we describe the synthesis of a full set of homo- and heterodimers of three intact structures of different ribosome-targeting antibiotics: tobramycin, clindamycin, and chloramphenicol. Several aspects of the biological activity of the dimeric structures were evaluated including antimicrobial activity, inhibition of in vitro bacterial protein translation, and the effect of dimerization on the action of several bacterial resistance mechanisms that deactivate tobramycin and chloramphenicol. This study demonstrates that covalently linking two identical or different ribosome-targeting antibiotics may lead to (i) a broader spectrum of antimicrobial activity, (ii) improved inhibition of bacterial translation properties compared to that of the parent antibiotics, and (iii) reduction in the efficacy of some drug-modifying enzymes that confer high levels of resistance to the parent antibiotics from which the dimers were derived.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.